Pharmacokinetics of theophyline metabolites in 8 Chinese patients

• 作 者: 曹文 卓海通 陈刚 凌树森
• 机 构: 金陵医院临床药理科
• 出 处: Acta Pharmacologica Sinica
• 发表日期: 2004年期
• 关键词: 甲基黄嘌呤 药物动力学 主要代谢产物 中间代谢产物 翌晨 消除率

目的：研究病人常规剂量茶碱治疗后代谢物的动力学．方法：病人静滴茶碱（６６μｍｏｌ·ｋｇ－１）．ＨＰＬＣ法测定给药前后２４ｈ茶碱及其代谢物：１，３二甲基尿酸（ＤＭＵＡ），３甲基黄嘌呤（３ＭＸ），１甲基尿酸（ＭＵＡ），中间代谢产物１甲基黄嘌呤（１ＭＸ）的浓度．结果：ＤＭＵＡ是代谢物中浓度最高的．３ＭＸ的清除速率最低．１ＭＸ很快转化成ＭＵＡ，体内浓度很低，但是，翌晨，１ＭＸ又回升到一个较高的浓度（从００４μｍｏｌ·Ｌ－１上升到１０５μｍｏｌ·Ｌ－１）．结论：ＤＭＵＡ是茶碱的主要代谢产物；在夜间１ＭＸ浓度积蓄，这是茶碱在夜间消除率下降的原因之一．

OBJECTIVE: To study the kinetics of metabolites after routine theophylline treatment in patients. Methods: Patients were intravenous hypophylline (6  6μmol · kg-1). Determination of theophylline and its metabolites: 1,3-dimethyl uric acid (DMUA), 3-methylxanthine (3MX), 1methyl uric acid (MUA), intermediate metabolites 1  methyl xanthine (1  MX) concentration. Results: DMUA is the highest metabolite concentration. 3  MX removal rate of the lowest. 1MX was quickly converted to MUA, and the body concentration was very low. However, 1MX returned to a higher concentration (from 0. 04 μmol·L-1 to 105 μmol·L-1) the next morning. Conclusion: DMUA is the main metabolite of theophylline; 1 × MX concentration at night savings, which is theophylline elimination rate at night one of the reasons.